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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Polo-like Kinase (PLK)-CFI-400945 fumarate
CFI-400945 fumarate

Chemical Structure : CFI-400945 fumarate

CAS No.: 1616420-30-4

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CFI-400945 fumarate (CFI400945, Ocifisertib)

货号: PC-63238Not For Human Use, Lab Use Only.

CFI-400945 (Ocifisertib) fumarate is a potent, highly selective, orally available PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM.

规格 价格 库存 数量
10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CFI-400945 (Ocifisertib) fumarate is a potent, highly selective, orally available PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM.
CFI-400945 causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM).
CFI-400945 significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

物理化学性质&存储条件

分子量 650.732
分子式 C37H38N4O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 166.66 mg/mL
Chemical Name/SMILES

Spiro[cyclopropane-1,3'-[3H]indol]-2'(1'H)-one, 2-[3-[(1E)-2-[4-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5'-methoxy-, (1R,2S)-, fumarate

参考文献

1. Sampson PB, et al. J Med Chem. 2015 Jan 8;58(1):147-69.

2. Mason JM, et al. Cancer Cell. 2014 Aug 11;26(2):163-76.

3. Lohse I, et al. Oncotarget. 2017 Jan 10;8(2):3064-3071.

4. Kawakami M, et al. Proc Natl Acad Sci U S A. 2018 Feb 20;115(8):1913-1918.

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